Assay Detail
Binding
CHEMBL1003027
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GARFTase in human KB cells assessed as inhibition of incorporation of [14C]glycine into [14C]formyl GAR after 30 mins in presence of azaserine
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | KB |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Trifunctional purine biosynthetic protein adenosine-3 (CHEMBL3972) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and biological activity of a novel series of 6-substituted thieno[2,3-d]pyrimidine antifolate inhibitors of purine biosynthesis with selectivity for high affinity folate receptors over the reduced folate carrier and proton-coupled folate transporter for cellular entry.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.69 | 7.88 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL491104 | — | — | 1 | 7.88 |
| CHEMBL490934 | — | — | 1 | 7.86 |
| CHEMBL34412 | LOMETREXOL | 2.0 | 1 | 7.85 |
| CHEMBL491129 | — | — | 1 | 7.63 |
| CHEMBL491298 | — | — | 1 | 7.58 |
| CHEMBL225072 | PEMETREXED | 4.0 | 1 | 7.52 |
| CHEMBL522455 | — | — | 1 | 7.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL491104 | — | IC50 | = | 13.3 | nM | 7.88 |
| CHEMBL490934 | — | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL34412 | LOMETREXOL | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL491129 | — | IC50 | = | 23.6 | nM | 7.63 |
| CHEMBL491298 | — | IC50 | = | 26.6 | nM | 7.58 |
| CHEMBL225072 | PEMETREXED | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL522455 | — | IC50 | = | 32.3 | nM | 7.49 |